AU2012347396B2 - 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives - Google Patents

5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives Download PDF

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Publication number
AU2012347396B2
AU2012347396B2 AU2012347396A AU2012347396A AU2012347396B2 AU 2012347396 B2 AU2012347396 B2 AU 2012347396B2 AU 2012347396 A AU2012347396 A AU 2012347396A AU 2012347396 A AU2012347396 A AU 2012347396A AU 2012347396 B2 AU2012347396 B2 AU 2012347396B2
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Australia
Prior art keywords
fluoro
compound
dementia
mmol
oxazin
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Ceased
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AU2012347396A
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AU2012347396A1 (en
Inventor
Henricus Jacobus Maria Gijsen
Sven Franciscus Anna Van Brandt
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2012347396A 2011-12-06 2012-12-04 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives Ceased AU2012347396B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11192171 2011-12-06
EP11192171.4 2011-12-06
PCT/EP2012/074349 WO2013083556A1 (en) 2011-12-06 2012-12-04 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives

Publications (2)

Publication Number Publication Date
AU2012347396A1 AU2012347396A1 (en) 2014-05-08
AU2012347396B2 true AU2012347396B2 (en) 2017-02-16

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AU2012347396A Ceased AU2012347396B2 (en) 2011-12-06 2012-12-04 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives

Country Status (12)

Country Link
US (1) US20140364428A1 (enExample)
EP (1) EP2788335B1 (enExample)
JP (1) JP5989130B2 (enExample)
KR (1) KR102002345B1 (enExample)
CN (1) CN103974940B (enExample)
AU (1) AU2012347396B2 (enExample)
CA (1) CA2853891C (enExample)
EA (1) EA024716B1 (enExample)
ES (1) ES2582473T3 (enExample)
IL (1) IL232917A (enExample)
MX (1) MX357383B (enExample)
WO (1) WO2013083556A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009258496B8 (en) 2008-06-13 2014-06-26 Shionogi & Co., Ltd. Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity
UA110467C2 (uk) 2009-12-11 2016-01-12 Шионогі Енд Ко., Лтд. Похідні оксазину
PH12012502377A1 (en) 2010-06-09 2014-10-14 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
NZ610948A (en) 2010-12-22 2014-06-27 Janssen Pharmaceutica Nv 5,6-dihydro-imidazo[1,2-a]pyrazin-8-ylamine derivatives useful as inhibitors of beta-secretase (bace)
BR112013022917A2 (pt) 2011-03-09 2016-12-06 Janssen Pharmaceutica Nv derivados 3,4-dihidro-pirrolo[1,2-a]pirazino-1-ilamina úteis como inibidores de beta-secretase (bace)
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну
EP2912035A4 (en) 2012-10-24 2016-06-15 Shionogi & Co DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY
JP6325092B2 (ja) 2013-06-12 2018-05-16 ヤンセン ファーマシューティカ エヌ.ベー. βーセクレターゼ(BACE)の阻害剤としての4−アミノ−6−フェニル−5,6−ジヒドロイミダゾ[1,5−A]ピラジン誘導体
KR102243133B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-6,7-디하이드로[1,2,3]트리아졸로[1,5-a]피라진 유도체
KR102243135B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진-3(2h)-온 유도체
EP3233834B1 (en) 2014-12-18 2019-11-13 Janssen Pharmaceutica NV 2,3,4,5-tetrahydropyridin-6-amine and 3,4-dihydro-2h-pyrrol-5-amine derivatives useful as inhibitors of beta-secretase
US20190359609A1 (en) * 2016-12-16 2019-11-28 Janssen Pharmaceutica Nv Bicyclic oga inhibitor compounds
WO2019025250A1 (en) 2017-08-04 2019-02-07 Basf Se SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
CN108440320A (zh) * 2018-05-09 2018-08-24 上海凌凯医药科技有限公司 一种高手性选择性合成α-双取代α-氨基酸的方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2011020806A1 (en) * 2009-08-19 2011-02-24 F. Hoffmann-La Roche Ag 3-amino-5-phenyl-5,6-dihydro-2h-[1,4]oxazine derivatives
WO2011071135A1 (ja) * 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
WO2011154431A1 (en) * 2010-06-09 2011-12-15 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2476605T3 (es) * 2007-04-24 2014-07-15 Shionogi & Co., Ltd. Derivados de aminohidrotiazina sustituidos con grupos cíclicos
JP5383483B2 (ja) * 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
US20120238557A1 (en) * 2009-11-13 2012-09-20 Shionogi & Co., Ltd. Aminothiazine or aminooxazine derivative having amino linker
US9242943B2 (en) * 2011-01-18 2016-01-26 Siena Biotech S.P.A. 1,4 oxazines as BACE1 and/or BACE2 inhibitors
IN2014DN03206A (enExample) * 2011-10-13 2015-05-22 Novartis Ag
UA111749C2 (uk) * 2011-12-05 2016-06-10 Янссен Фармацевтика Нв Похідні 6-дифторметил-5,6-дигідро-2h-[1,4]оксазин-3-аміну

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011009943A1 (en) * 2009-07-24 2011-01-27 Novartis Ag Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders
WO2011020806A1 (en) * 2009-08-19 2011-02-24 F. Hoffmann-La Roche Ag 3-amino-5-phenyl-5,6-dihydro-2h-[1,4]oxazine derivatives
WO2011071135A1 (ja) * 2009-12-11 2011-06-16 塩野義製薬株式会社 オキサジン誘導体
WO2011154431A1 (en) * 2010-06-09 2011-12-15 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)

Also Published As

Publication number Publication date
KR20140106541A (ko) 2014-09-03
EA024716B1 (ru) 2016-10-31
NZ623858A (en) 2015-05-29
HK1198535A1 (en) 2015-05-15
CA2853891C (en) 2020-03-10
CA2853891A1 (en) 2013-06-13
EP2788335A1 (en) 2014-10-15
MX2014006752A (es) 2014-07-14
IL232917A (en) 2016-07-31
MX357383B (es) 2018-07-06
ES2582473T3 (es) 2016-09-13
IL232917A0 (en) 2014-08-03
US20140364428A1 (en) 2014-12-11
CN103974940B (zh) 2016-08-24
AU2012347396A1 (en) 2014-05-08
CN103974940A (zh) 2014-08-06
KR102002345B1 (ko) 2019-07-22
JP5989130B2 (ja) 2016-09-07
WO2013083556A1 (en) 2013-06-13
EP2788335B1 (en) 2016-04-13
EA201491102A1 (ru) 2014-09-30
JP2015500257A (ja) 2015-01-05

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